| + |
Phenelzine | down-regulates activity 
chemical inhibition
|
SLC6A2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258743 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 9537821 |
At the human norepinephrine transporter, among the antidepressants desipramine was the most potent with a KD=0.83±0.05 nM. All the tetracyclic antidepressants, except mirtazapine, which is a structural analog of mianserin, were more potent at the norepinephrine transporter than at the serotonin transporter. Tomoxetine, considered from animal data to be very selective for the norepinephrine transporter, had high affinity for the human norepinephrine transporter (KD=2.03±0.06 nM). However, at the human serotonin transporter, tomoxetine was nearly as potent and close to that for dothiepin and venlafaxine. Venlafaxine, considered a serotonin and norepinephrine re-uptake inhibitor based on animal data, was very weak at the human norepinephrine transporter. Its KD value was 5× less that than for norepinephrine. All of the serotonin selective re-uptake inhibitors, with the exception of paroxetine, were also weak at the human norepinephrine transporter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Phenelzine | down-regulates activity
chemical inhibition
|
MAOA |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257777 |
|
|
in vitro |
|
| pmid |
sentence |
| 18426226 |
Phenylethylhydrazine stoichiometrically reduces the covalent FAD moieties of MAO A and of MAO B. Molecular oxygen is required for the inhibition reactions, and the level of O2 consumption for phenylethylhydrazine is 6-7-fold higher with either MAO A or MAO B than for the corresponding reactions with benzylhydrazine or phenylhydrazine. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
Phenelzine | down-regulates activity
chemical inhibition
|
MAOB |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257778 |
|
|
in vitro |
|
| pmid |
sentence |
| 18426226 |
Phenylethylhydrazine stoichiometrically reduces the covalent FAD moieties of MAO A and of MAO B. Molecular oxygen is required for the inhibition reactions, and the level of O2 consumption for phenylethylhydrazine is 6-7-fold higher with either MAO A or MAO B than for the corresponding reactions with benzylhydrazine or phenylhydrazine. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
Phenelzine | down-regulates activity
chemical inhibition
|
SLC6A3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258745 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 9537821 |
At the human dopamine transporter, sertraline and nomifensine were the most potent with KD's of 25±2 and 56±3, respectively. Except for these two compounds, most antidepressants were not potent at the human dopamine transporter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Phenelzine | down-regulates activity
chemical inhibition
|
SLC6A4 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258744 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 9537821 |
Among the antidepressants that we tested, paroxetine, which is a serotonin selective re-uptake inhibitor based on animal data, was the most potent for the human serotonin transporter with a KD=0.13±0.01 nM. Some tricyclic antidepressants (clomipramine, imipramine and amitriptyline), as well as some other antidepressants (sertraline, fluoxetine, citalopram and fluvoxamine) and some of their metabolites (norfluoxetine, desmethylsertraline and desmethylcitalopram) were also very potent at the human serotonin transporter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
Phenelzine
